What question did this study set out to answer?

Synthesize a series of derivatives based on a novel bicyclo[2.2.1]heptane thromboxane receptor antagonist and evaluate their in vitro biological profiles.

September 1, 1988Journal of Medicinal Chemistry

Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (.+-.)-(5Z)-7-3-endo[(phenylsulfonyl)aminobicyclo2.2.1hept-2-exo-yl]heptenoic acid

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Population

in vitro models

Design

Preclinical

Authors

MNMasayuki NarisadaShionogi (Japan)MOMitsuaki OhtaniShionogi (Japan)FWFumihiko WatanabeFukushima Medical University

Discussion

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Implication

No clinical implications yet; leaves open whether these derivatives advance thromboxane antagonism beyond current agents.

Key Points

Synthesize a series of derivatives based on a novel bicyclo[2.2.1]heptane thromboxane receptor antagonist and evaluate their in vitro biological profiles.
Synthesized diverse derivatives of (+/-)-(5Z)-7-[3-endo[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]heptenoic acid via chemical modification.
Assessed in vitro thromboxane receptor antagonist activity against platelet aggregation and vascular smooth muscle contraction.
Generated novel sulfonamide-substituted bicyclo[2.2.1]heptyl heptenoic acid analogs with distinct stereochemical configurations.
Identified derivatives exhibiting strong antagonistic affinity toward thromboxane A2 receptors in vitro.

Structured PICO

Population

in vitro models

Intervention

derivatives of a novel thromboxane receptor antagonist, (.+-.)-(5Z)-7-[3-endo[(phenylsulfonyl)amino]bicyclo[2.2.1]hept-2-exo-yl]heptenoic acid

Outcome

in vitro activitysurrogate

The paper describes the synthesis and in vitro activity of derivatives of a novel thromboxane receptor antagonist.

Cite This Study

Narisada et al. (1988) studied this question.

synapsesocial.com/papers/6a945bd3fde2ed39e1a0d003 https://doi.org/10.1021/jm00117a028

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Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (.+-.)-(5Z)-7-3-endo[(phenylsulfonyl)aminobicyclo2.2.1hept-2-exo-yl]heptenoic acid

Discussion

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Implication

Key Points

Structured PICO

Cite This Study

Synthesis and in vitro activity of various derivatives of a novel thromboxane receptor antagonist, (.+-.)-(5Z)-7-3-endo[(phenylsulfonyl)aminobicyclo2.2.1hept-2-exo-yl]heptenoic acid

Discussion

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Implication

Key Points

Structured PICO

Cite This Study

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